Sugerlin (Prasugrel), a thienopyridine derivative, is a platelet activation and aggregation inhibitor structurally and pharmacologically related to Clopidogrel and Ticlopidine. Similar to Clopidogrel, Sugerlin is a prodrug that requires enzymatic transformation in the liver to its active metabolite, irreversibly binds to P2Y12 type ADP receptors on platelets thus preventing activation of the GPIIb/IIIa receptor complex. As a result, inhibition of ADP-mediated platelet activation and aggregation occurs. In combination with acetylsalicylic acid (ASA) to prevent atherothrombotic events in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI). May be used in patients with unstable angina (UA), non-ST elevation myocardial infarction (NSTEMI), ST-elevation myocardial infarction (STEMI) who are to be managed with PCI. sugerlin is not recommended in patients 75 years of age or greater, those that weigh<60kg, and patients with a history of stroke or transient ischemic attack due to increased risk of fatal and intracranial bleeding.
79% or greater of the dose is absorbed after oral administration. Absorption and metabolism occur rapidly and peak plasma concentrations (C max) are reached approximately 30 minutes following oral administration. Administration with a high fat, high calorie meal did not affect the AUC of the active metabolite in healthy individuals, but the C max was decreased by ~49% and the T max was increased to 0.5 to 1.5 hours sugerlin may be administered with or without food. Approximately 98% of the active metabolite was bound to human serum albumin in a 4% buffered solution. The major inactive metabolites are also highly bound to human plasma proteins.
Sugerlin is not detected in plasma following oral administration. It is rapidly hydrolyzed in the intestine to thiolactone by human carboxyl esterase (hCE) 2. This intermediate is further metabolized to its active metabolite, by cytochrome P450 enzymes in the liver (primarily CYP3A4 and CYP2B6 and to a lesser extent by CYP2C9 and CYP2C19). The active metabolite is further metabolized by S-methylation or cysteine conjugation to two inactive metabolites. Unlike Clopidogrel, transformation of Sugerlin to its active metabolite does not appear to be affected by cytochrome P450 polymorphisms.
Approximately 68% of the orally administered dose is excreted in urine and 27% in the feces, as inactive metabolites. The active metabolite is not expected to be removed by dialysis.
The active metabolite has an elimination half-life of about 7.4 hours (range 2-15 hours).
Usual Geriatric Dose for Acute Coronary Syndrome:
65 to less than 75 years:
-Initial dose: 60 mg orally once
-Maintenance dose: 10 mg orally once a day
75 years or older: Use is generally not recommended in such patients, except in high-risk situations (e.g., diabetes or prior myocardial infarction) when benefit outweighs risk.
Usual Adult Dose for Acute Coronary Syndrome:
Initial dose: 60 mg orally once
Maintenance dose: 10 mg orally once a day
-Aspirin 75 to 325 mg daily should be taken with this drug.
Comments:
-No clear benefit was observed when the loading dose of this drug was administered prior to diagnostic coronary angiography compared to at the time of percutaneous coronary intervention (PCI); however, risk of bleeding was increased with early administration in patients undergoing PCI or early coronary artery bypass graft surgery (CABG).

Use: To reduce the rate of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with PCI for unstable angina (UA), non-ST segment elevation myocardial infarction (NSTEMI), or ST segment elevation myocardial infarction (STEMI).
Interaction:
Acetazolamide: Acetazolamide may increase the excretion rate of sugerlin which could result in a lower serum level and potentially a reduction in efficacy.
Acetyl sulfisoxazole: The metabolism of sugerlin can be decreased when combined with Acetyl sulfisoxazole.
Acetylsalicylic acid: The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with sugerlin
Altrenogest : Altrenogest may decrease the anticoagulant activities of sugerlin
Amikacin :Amikacin may decrease the excretion rate of sugerlin which could result in a higher serum level.
Ammonium chloride :sugerlin may decrease the excretion rate of Ammonium chloride which could result in a higher serum level.
Amoxicillin: Amoxicillin may decrease the excretion rate of sugerlin which could result in a higher serum level.
Ampicillin: Ampicillin may decrease the excretion rate of sugerlin which could result in a higher serum level.
Apramycin: Apramycin may decrease the excretion rate of sugerlin which could result in a higher serum level.

US BOXED WARNING: BLEEDING RISK
-This drug can cause significant, sometimes fatal, bleeding.
-Do not use this drug in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke.cin: may decrease the excretion rate of sugerlin which could result in a higher serum patients 75 years or older, this drug is generally not recommended due to increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk situations (e.g., patients with diabetes or a history of myocardial infarction) where its effect appears to be greater and its use may be considered.
-Do not start this drug in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue this drug at least 7 days prior to any surgery.
-Additional risk factors for bleeding include: body weight less than 60 kg; propensity to bleed; concomitant use of medications that increase risk of bleeding (e.g., warfarin, heparin, fibrinolytic therapy, chronic use of non-steroidal anti-inflammatory drugs [NSAIDs]).
-Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of this drug.
-If possible, manage bleeding without discontinuing this drug. Discontinuation, particularly in the first few weeks after acute coronary syndrome, increases the risk of subsequent cardiovascular events.
Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.
Patient advice:
-Inform patients that they will bruise and bleed more easily and take longer than usual to stop bleeding.
-Advise patients to report any unanticipated, prolonged, or excessive bleeding or blood in their stool or urine.
-Advise patients to inform physicians and dentists that they are using this drug before any invasive procedure is scheduled or any new medication is taken.
-Remind patients not to discontinue this drug without first discussing with their physician.
-Instruct patients to seek immediate medical attention if they experience any of the following symptoms that cannot otherwise be explained as they may be signs of thrombotic thrombocytopenic purpura (TTP): fever, weakness, extreme skin paleness, and purple skin patches, yellowing of the skin or eyes, or neurological changes.